Details for Patent: 9,744,179

Title:	Tetracycline compositions
Abstract:	The present invention relates to compositions, pharmaceutical compositions, and methods for preparing the same, comprising a tetracycline with improved stability and solubility. Some embodiments include a tetracycline with an excess of a divalent or trivalent cation.
Inventor(s):	Griffith; David C. (San Marcos, CA), Boyer; Serge (San Diego, CA), Hecker; Scott (Del Mar, CA), Dudley; Michael N. (San Diego, CA)
Assignee:	Rempex Pharmaceuticals, Inc. (San Diego, CA)
Filing Date:	Dec 05, 2014
Application Number:	14/562,449
Claims:	1. A method of treating a bacterial infection, comprising administering a therapeutically effective amount of a pharmaceutical composition to a subject in need thereof via topical administration to the eye of the subject, the pharmaceutical composition comprising an aqueous solution of tigecycline and a divalent or trivalent metal cation, wherein the pH of the solution is greater than 4 and less than 7 and the molar ratio of divalent or trivalent metal cation to tigecycline is greater than 6:1. 2. The method of claim 1, wherein the molar ratio of divalent or trivalent metal cation to tigecycline is greater than 8:1. 3. The method of claim 1, wherein the molar ratio of divalent or trivalent metal cation to tigecycline is greater than 10:1. 4. The method of claim 1, wherein the molar ratio of divalent or trivalent metal cation to tigecycline is about 12:1. 5. The method of claim 1, wherein the divalent or trivalent metal cation is a divalent metal cation. 6. The method of claim 1, wherein the divalent or trivalent metal cation is calcium. 7. The method of claim 1, wherein the solution comprises calcium chloride or calcium sulfate. 8. The method of claim 1, wherein the divalent or trivalent metal cation is magnesium. 9. The method of claim 1, wherein the solution comprises magnesium sulfate or magnesium chloride. 10. The method of claim 1, wherein the concentration of tigecycline is at least 1 mg/ml. 11. The method of claim 1, wherein the concentration of tigecycline is 5 mg/ml. 12. The method of claim 1, wherein the solution comprises one or more additional constituents selected from the group consisting of hydrocortisone, dexamethasone, thonzonium bromide, tyloxapol, boric acid, and benzalkonium chloride. 13. The method of claim 1, wherein the solution does not comprise a component selected from the group consisting of an antioxidant, a pyridine-containing compound, gluconate, an alcohol, glycerol, polyethylene glycol, a pyrrolidone-containing compound, a water-miscible local anaesthetic, urea, lactose, and a dehydrating agent. 14. The method of claim 1, wherein the pharmaceutical composition is contained within a vial prior to administration. 15. The method of claim 14, wherein the vial is a single-use vial. 16. A method of treating a bacterial infection, comprising: reconstituting a water-soluble solid composition in a pharmaceutically acceptable diluent to form a solution; and administering a therapeutically effective amount of the solution to a subject in need thereof via topical administration to the eye of the subject, wherein the water-soluble solid composition comprises tigecycline and a divalent or trivalent metal cation, wherein the molar ratio of divalent or trivalent metal cation to tigecycline is greater than 6:1. 17. The method of claim 16, wherein the molar ratio of divalent or trivalent metal cation to tigecycline is greater than 8:1. 18. The method of claim 16, wherein the molar ratio of divalent or trivalent metal cation to tigecycline is greater than 10:1. 19. The method of claim 16, wherein the molar ratio of divalent or trivalent metal cation to tigecycline is about 12:1. 20. The method of claim 16, wherein the divalent or trivalent metal cation is a divalent metal cation. 21. The method of claim 16, wherein the divalent or trivalent metal cation is calcium. 22. The method of claim 16 comprising calcium chloride or calcium sulfate. 23. The method of claim 16, wherein the divalent or trivalent metal cation is magnesium. 24. The method of claim 16 comprising magnesium sulfate or magnesium chloride. 25. The method of claim 16, wherein the water-soluble solid composition is in the form of a lyophile. 26. The method of claim 16, wherein the water-soluble solid composition is contained within a vial. 27. The method of claim 26, wherein the vial is a single-use vial. 28. The method of claim 26, wherein the vial comprises greater than 30 mg and less than 100 mg of tigecycline. 29. The method of claim 26, wherein the vial comprises at least 50 mg of tigecycline. 30. The method of claim 26, wherein the vial comprises at least 200 .mu.g of tigecycline. 31. The method of claim 26, wherein the vial comprises at least 1 mg of tigecycline. 32. The method of claim 16, wherein the pharmaceutically acceptable diluent is water.